DL-aspartic acid dibutyl ester | 802842-54-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: DL-aspartic acid dibutyl ester
• 英文别名: DL-Asparaginsaeure-dibutylester；Di-n-Butyl-DL-aspartat；Dibutyl 2-Aminosuccinate；dibutyl 2-aminobutanedioate
• CAS: 802842-54-2
• 化学式: C₁₂H₂₃NO₄
• 分子量: 245.319
• InChiKey: MMJGQHYROJTOHX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  17
• 可旋转键数：
  11
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  78.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  DL-aspartic acid dibutyl ester 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 生成 (2RS)-2-aminobutane-1,4-diol
  参考文献：
  名称：

  潜在的抗辐射药物。3.2-氨基-2-烷基-1，3-丙二硫醇和3-氨基-4-巯基-1-丁醇。

  摘要：

  DOI：

  10.1021/jm00322a026
• 作为产物：
  描述：

  DL-天门冬氨酸 、 正丁醇 在 盐酸 作用下， 生成 DL-aspartic acid dibutyl ester
  参考文献：
  名称：

  潜在的抗辐射药物。3.2-氨基-2-烷基-1，3-丙二硫醇和3-氨基-4-巯基-1-丁醇。

  摘要：

  DOI：

  10.1021/jm00322a026

文献信息

• Multivalent indole compounds and use thereof as phospholipase-A2 inhibitors
  申请人：Chang Han-Ting

  公开号：US20070135385A1

  公开（公告）日：2007-06-14

  Indole and indole-related compounds, compositions and methods are disclosed. The compounds of the invention are useful as phospholipase inhibitors. The compounds and compositions of the invention are useful for treatment of phospholipase-related conditions, such as insulin-related, weight-related and/or cholesterol-related conditions in an animal subject.

  吲哚和与吲哚相关的化合物、组合物以及方法被披露。发明中的这些化合物作为磷脂酶抑制剂非常有用。发明中的这些化合物和组合物用于治疗动物受试者中的磷脂酶相关状况，例如胰岛素相关、体重相关和/或胆固醇相关状况。
• Phospholipase inhibitors, including multi-valent phospholipase inhibitors, and use thereof, including as lumen-localized phospholipase inhibitors
  申请人：Chang Han-Ting

  公开号：US20070135383A1

  公开（公告）日：2007-06-14

  The present invention provides methods and compositions for the treatment of phospholipase-related conditions. In particular, the invention provides a method of treating insulin-related, weight-related conditions and/or cholesterol-related conditions in an animal subject. The method generally involves the administration of a non-absorbed and/or effluxed phospholipase A2 inhibitor that is localized in a gastrointestinal lumen.

  本发明提供了治疗磷脂酶相关疾病的方法和组合物。具体地，本发明提供了一种用于治疗动物主体中的胰岛素相关、体重相关和/或胆固醇相关疾病的方法。该方法通常涉及在胃肠道腔中定位的非吸收和/或外流的磷脂酶A2抑制剂的给药。
• TRICARBONYL TECHNETIUM-99m OR RHENIUM-188 LABELED CYCLIC RGD DERIVATIVES, A PREPARATION METHOD THEREOF, AND A PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVES AS AN ACTIVE INGREDIENT FOR USE IN THE DIAGNOSIS OR TREATMENT OF ANGIOGENESIS-RELATED DISEASES
  申请人：Lee Byung Chul

  公开号：US20130064766A1

  公开（公告）日：2013-03-14

  The present invention relates to tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives, a preparation method thereof, and a pharmaceutical composition containing the derivative as an active ingredient for use in the diagnosis or treatment (radiotherapy) of angiogenesis-related diseases. The tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives of the present invention has a high subnanomolar affinity to integrin α v β 3 (also called as a vitronectin receptor) that is activated in an angiogenic action induced by a tumor, reflects a high tumor image of the tricatvonyl technetium-99m labeled cyclic RGD derivative after initial intake in an animal in which cancer cells are transplanted, and acts exclusively upon cancer cells having selectively activated integrin α v β 3 because of a substantially low intake into the liver and intestines, compared to existing known radioactive isotope labeled cyclic RGD derivatives. These results show that the rhenium-188 labeled derivative, a therapeutic nuclide using the same precursor as used in the technetium-99m labeling, effectively inhibits the growth of a tumor and demonstrates therapeutic efficacy when administered via tail vein injection to an animal model bearing tumor, compared to a case where only saline has been injected, thereby making it useful as a medicine for the diagnosis or treatment of angiogenesis-related diseases.

  本发明涉及三羰基锝-99m或铼-188标记的环状RGD衍生物，其制备方法以及含有该衍生物作为活性成分的药物组合物，用于诊断或治疗与血管生成相关的疾病（放射治疗）。本发明的三羰基锝-99m或铼-188标记的环状RGD衍生物具有与整合素αvβ3（也称为玻璃蛋白连接受体）的高亚纳摩尔亲和力，该受体在肿瘤诱导的血管生成作用中被激活，反映了在移植了癌细胞的动物中，三羰基锝-99m标记的环状RGD衍生物具有高肿瘤成像，且与现有已知的放射性同位素标记的环状RGD衍生物相比，仅对选择性激活整合素αvβ3的癌细胞起作用，因肝脏和肠道的摄取量明显低于现有已知的放射性同位素标记的环状RGD衍生物。这些结果表明，使用与锝-99m标记相同的前体制备的铼-188标记衍生物，有效抑制肿瘤的生长，并在通过尾静脉注射给患有肿瘤的动物模型时表现出治疗效果，与仅注射生理盐水的情况相比，因此可用作诊断或治疗与血管生成相关的疾病的药物。
• NITROIMIDAZOLE-AMINO ACID COMPOUND TYPE NUCLIDE HYPOXIA IMAGING AGENT AND INTERMEDIATES FOR PREPARING THEM
  申请人：Ruan, Jianping

  公开号：EP2366693A1

  公开（公告）日：2011-09-21

  Nitroinidazole-amino acid compound type nuclide hypoxia imaging agents, intermediates for preparing them, and a process for preparing the intermediates, and their use as a medicament, especially for cerebral thrombosis, tumor and other hypoxic lesions such as imaging contrast agent of ulcer or blood embolism.

  硝基咪唑-氨基酸化合物型核素缺氧成像剂、制备中间体和制备中间体的工艺及其作为药物的用途，特别是用于脑血栓、肿瘤和其他缺氧病变，如溃疡或血液栓塞的成像造影剂。
• Process for preparing pyridine-2,3- dicarboxylic acid compounds
  申请人：Daiso Co., Ltd.

  公开号：EP0299362B1

  公开（公告）日：1991-12-04